2-benzoylimidazopyridine derivatives, preparation and therapeutic use thereof
    2.
    发明授权
    2-benzoylimidazopyridine derivatives, preparation and therapeutic use thereof 失效
    2-苯甲酰基咪唑并吡啶衍生物,其制备和治疗用途

    公开(公告)号:US07902219B2

    公开(公告)日:2011-03-08

    申请号:US12336989

    申请日:2008-12-17

    IPC分类号: A61K31/437 C07D471/04

    CPC分类号: C07D471/04

    摘要: The present invention is related to a compound of formula (I) wherein R1, R2, R3, R4 and X are as defined herein, or an acid-addition salt thereof, its preparation and therapeutic use in the treatment or prevention of diseases involving the Nurr-1 nuclear receptors, also known as NR4A2, NOT, TINUR, RNR-1 and HZF3.

    摘要翻译: 本发明涉及其中R 1,R 2,R 3,R 4和X如本文所定义的式(I)化合物或其酸加成盐,其在治疗或预防涉及 Nurr-1核受体,也称为NR4A2,NOT,TINUR,RNR-1和HZF3。

    Process for preparing 3-fluoroquinolines
    5.
    发明授权
    Process for preparing 3-fluoroquinolines 失效
    制备3-氟喹啉的方法

    公开(公告)号:US07396934B2

    公开(公告)日:2008-07-08

    申请号:US10985533

    申请日:2004-11-10

    IPC分类号: C07D215/38 C07D215/18

    摘要: The invention relates to a novel preparation of 3-fluoroquinolines of formula (I) in which R1, R2, R3 and R4 represent: a) a fluorine; b) an alkyl optionally substituted with one to three fluorines, with OR5 in which R5 is an alkyl, a hydrogen or a hydroxyl-protecting group, or with NR′R″ in which R′ and R″ represent an alkyl, a hydrogen or an amino-protecting group; c) OR6 in which R6 represents a hydrogen, a phenol-protecting group or an alkyl, optionally substituted with a fluorine, with OR5 or with NR′R″ as defined above; d) NR′1R″1 in which R′1 and R″1 have the values of R′ et R″ or represent an alkyl substituted with a fluorine, with OR5 or NR′R″ as defined above; e) CO2Ra, in which Ra represents hydrogen, alkyl or a carboxyl-protecting group, and also novel intermediate compounds. The quinolines of formula (I) are intermediates useful in the preparation of compounds having antibacterial activity, described in particular in applications WO 02/40474 or WO 02/72572.

    摘要翻译: 本发明涉及式(I)的3-氟喹啉的新型制备方法,其中R 1,R 2,R 3和R 3, 代表:a)氟; b)任选被一至三个氟取代的烷基,其中R 5是烷基,氢或羟基保护基或NR' 其中R'和R“表示烷基,氢或氨基保护基的”R“ c)OR 6其中R 6表示氢,苯酚保护基或任选被氟取代的烷基,OR 5或N >或如上定义的NR'R“ d)NR'1 R“1其中R'1和R”1 <1的数值为 或者代表被氟取代的烷基,其具有如上定义的OR 5或NR'R“; e)其中R aa代表氢,烷基或羧基保护基,以及新的中间体化合物的CO 2 CO 2。 式(I)的喹啉是可用于制备具有抗菌活性的化合物的中间体,特别在申请WO 02/40474或WO 02/72572中有所描述。